Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
  • Patent number: 5658940
    Abstract: Novel succinimides and maleimides are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-3-(3",4"-dimethoxyphenyl)propionate.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: August 19, 1997
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5639752
    Abstract: Compounds of the formula ##STR1## wherein Z is ##STR2## R.sub.1 is ##STR3## X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
    Type: Grant
    Filed: May 20, 1994
    Date of Patent: June 17, 1997
    Assignee: Pfizer Inc
    Inventor: John Eugene Macor
  • Patent number: 5633254
    Abstract: Synergistic mixtures which include dimethomorph and cymoxonil in a fungicidially effective aggregate amount, and the use of such mixtures in the control of plant diseases. In certain embodiments, a contact fungicide is included, along with the dimethomorph and cymoxonil in suitable ratios.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: May 27, 1997
    Assignees: Agrogene Ltd., C.T.S. Ltd.
    Inventor: Yigal Cohen
  • Patent number: 5605923
    Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: February 25, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 5605914
    Abstract: Cyclic imides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-(2,6-dioxo-3-piperidinyl)-4-azaisoindoline-1,3-dione.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: February 25, 1997
    Assignee: Celgene Corporation
    Inventor: George W. Muller
  • Patent number: 5593990
    Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: January 14, 1997
    Assignee: The Children's Medical Center Corporation
    Inventor: Robert D'Amato
  • Patent number: 5536723
    Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: July 16, 1996
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5534533
    Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: July 9, 1996
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Toshiyuki Kato, Yozo Hori
  • Patent number: 5527547
    Abstract: Improved biocidal composition and method for controlling biofouling and microorganism population levels in recirculating water systems such as cooling towers, swimming pools or spas is disclosed and claimed. The composition comprises a hypochlorite donor and a bromide ion donor in proportions selected to maintain a mole ratio of the sum of all bromine containing species to the sum of all hypohalite species in the recirculating water of about 0.2 to about 20. The method comprises introducing into the recirculating water a mixture or combination of a hypochlorite donor and a bromide ion donor in an amount sufficient to maintain a ratio of the sum of all bromine containing species to the sum of all species in the recirculating water in the range of about 0.2 to about 20.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: June 18, 1996
    Assignee: The University of Houston
    Inventors: Terry V. T. Hight, Jack V. Matson, Lawrence F. Rakestraw, Zhihe Zhang, Thomas C. Kuechler
  • Patent number: 5500441
    Abstract: A fungicidal mixture containinga) the oxime ether carboxamide of the formula I ##STR1## and b) a phthalimide derivative selected from the group of compounds II and III ##STR2## in a synergistically active amount is described.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: March 19, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Reinhold Saur, Klaus Schelberger, Manfred Hampel
  • Patent number: 5491144
    Abstract: Compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: February 13, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Uwe Trinks, Peter Traxler
  • Patent number: 5470586
    Abstract: A method of controlling the attachment of organisms to an underwater surface is disclosed. The method comprises contacting the organisms with a compound of Formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halogen, or hydroxyl. Antifouling coatings and cementitious compositions containing a compound of Formula I are also disclosed.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: November 28, 1995
    Assignee: Duke University
    Inventor: Donald J. Gerhart
  • Patent number: 5464854
    Abstract: The method of treatment moderating, blocking and/or eliminating premenstrual syndrome embodies the intermittent administering of an AT1 antagonist to a female having menstrual cycles characterized predominately by during substantially the luteal phase inclusive of at least one and frequently by two or more affective and/or autonomic and/or somatic symptoms of substantially incapacitating severity(ies) proximately substantially prior to menses of a menstrual cycle. Losartan is an example of an AT1 inhibitor and is administered either orally or parenterally continuously to a female during her menstrual cycle's luteal phase.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: November 7, 1995
    Inventor: Anathony S. dePadova
  • Patent number: 5455261
    Abstract: The present invention relates to a process for the control of fungal disease of plants by applying to the leaves of the plants:a) 2-(4-chlorobenzylidene)-5,5-diemthyl-1-(1H-1, 2,4-triazol-1-ylmethyl)-1-cyclopentanol;b) one or more fungicides suitable for protecting against the said fungal diseases and to compositions which may be used in the process.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: October 3, 1995
    Assignee: Rhone-Poulenc Secteur Agrochimie
    Inventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
  • Patent number: 5447929
    Abstract: Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5439940
    Abstract: The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: August 8, 1995
    Assignee: EGIS Gyogyszergyar Rt.
    Inventors: Klara Reiter nee Eszes, Zoltan Budai, Tibor Mezei, Gabor Blasko, Gyula Simig, Istvan Gyertyan, Luiza Petocz, Marton Fekete, Katalin Szemeredi, Istvan Gacsalyi, Gabor Gigler, Ludmilla Rohacas nee Zamkovaja, Maria Szecsey nee Hegedus, Eniko Szirt nee Kiszelly
  • Patent number: 5409885
    Abstract: Stable and flowable aqueous dispersions of at least one water-insoluble material are formulated by dispersing such water-insoluble material, e.g., solid particulates of a plant protection compound, into a homogeneous, stable and flowable aqueous composition that includes (1) at least one water-soluble derivative of a plant protection active agent bearing at least one ionizable functional group and at least one hydrophilic functional group, (2) at least one nonionic surface-active agent and/or at least one aliphatic, cycloaliphatic or arylaliphatic alcohol having from 4 to 15 carbon atoms, and (3) water, this composition exhibiting optical birefringence and a yield point of at least 0.1 pascal.
    Type: Grant
    Filed: July 9, 1992
    Date of Patent: April 25, 1995
    Assignee: Rhone-Poulenc Chimie
    Inventors: Paul-Joel Derian, Gilles Guerin, Philippe Jost
  • Patent number: 5389668
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: February 14, 1995
    Assignee: Adir Et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5376673
    Abstract: Isoindole compounds of the formula (I) ##STR1## wherein R.sub.1 represents hydrogen; C.sub.1 -C.sub.6 alkyl; benzyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, methylenedioxy; C.sub.2 -C.sub.8 aliphatic acyl; benzoyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, methylenedioxy;R.sub.2 -R.sub.3 are selected independently from hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; trifluoromethyl; hydroxy; nitro; amino; mono or di C.sub.1 -C.sub.4 alkylamino; cyano; C.sub.1 -C.sub.6 alkoxy; C.sub.2 -C.sub.6 alkoxycarbonyl;Y is ethylene, or a straight or branched alkylene chain containing from 3 to 6 carbon atoms, and the salts thereof of pharmaceutically acceptable acids. The compounds possess antianginal activity and are used in the preparation of medicaments for antianginal therapy.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: December 27, 1994
    Assignee: Italfarmaco S.p.A.
    Inventors: Alberto Sala, Silvio Levi, Francesca Benedini, Roberta Cereda, Piero Soldato
  • Patent number: 5326760
    Abstract: Aminobutanoic acids of the following formula (I): ##STR1## where R.sup.1 -R.sup.5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).
    Type: Grant
    Filed: March 15, 1993
    Date of Patent: July 5, 1994
    Assignee: Glaxo, Inc.
    Inventors: Andrew B. McElroy, Peter J. Brown, David H. Drewry, James M. Salovich, Frank J. Schoenen
  • Patent number: 5310751
    Abstract: All possible stereoisomer forms and mixtures thereof of a compound of the formula ##STR1## wherein X is halogen, Y is --0-- or --S-- and R is selected from the group consisting of optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, optionally substituted aryl and aralkyl of up to 14 carbon atoms and optionally substituted heterocyclic having pesticidal properties.
    Type: Grant
    Filed: July 1, 1992
    Date of Patent: May 10, 1994
    Assignee: Roussel Uclaf
    Inventors: Didier Babin, Marc Benoit, Jacques Demassey, Jean-Pierre Demoute
  • Patent number: 5292759
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY is O, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: March 8, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5281617
    Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: January 25, 1994
    Assignee: Cortech, Inc.
    Inventors: Gary P. Kirschenheuter, John C. Cheronis
  • Patent number: 5266587
    Abstract: The invention provides a new sub-class or organic peroxyacids comprising N-alkyl substituted peroxytrimellitimide of formula (I) in which R=hydrogen or linear or branched alkyl, which demonstrates an excellent combination of safe-handling and bleach performance rendering the sub-class particularly suitable for use as bleach and/or disinfectant in various bleach, bleach additive or washing compositions. Effective bleaching peroxyacids include those in which R=n propyl, iso-propyl, n butyl, sec-butyl, n pentyl and n heptyl. The invention also comprises processes for making the peroxyacids, compositions containing them and processes for washing and/or bleaching and/or disinfecting employing the invention peroxyacids or compositions containing them.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: November 30, 1993
    Assignee: Interox Chemicals Limited
    Inventors: John P. Sankey, A. Pryce James
  • Patent number: 5262533
    Abstract: Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.
    Type: Grant
    Filed: May 6, 1992
    Date of Patent: November 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Peter J. Sinclair, Helen M. Organ, Matthew J. Wyvratt
  • Patent number: 5256686
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined in the specification, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: October 26, 1993
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5238690
    Abstract: The present invention relates to a novel biologically pure culture of Triderma Harzianum, I-952, to biological control compositions containing same and to methods of protecting plants from the disease gray mold, caused by B. Cinera and the disease white rot caused by S. Sclerotiorum with such compositions.
    Type: Grant
    Filed: July 10, 1991
    Date of Patent: August 24, 1993
    Assignees: Peri Applications (1885) Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Yigal Elad, Gilly Zimand, Ilan Chet
  • Patent number: 5180420
    Abstract: The water dispersible granule of the present invention contains (a) a pesticidal active ingredient which is solid at room temperature, (b) an anionic surface active agent, and (c) a kaolin series clay having a volume median diameter of 2 .mu.m or more, and it exhibits a good disintegrability-in-water and a high dispersion stability.
    Type: Grant
    Filed: March 11, 1991
    Date of Patent: January 19, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yasuyuki Katayama, Yasuhiko Ishimoto, Fumio Horide, Shigenori Tsuda, Fumio Nishioka
  • Patent number: 5118704
    Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: June 2, 1992
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 5102447
    Abstract: The present invention relates to methods for protecting crop plants from undesirable effects of pesticides and herbicides. The roots, seeds or soil surrounding the crop plants are treated with an effective amount of phthalimide compound in conjunction with the use of an effective amount of the insecticidal compound or herbicidal compound. Compositions for so protecting crop plants also are provided.
    Type: Grant
    Filed: November 6, 1989
    Date of Patent: April 7, 1992
    Assignee: American Cyanamid Company
    Inventor: Donald W. Gates
  • Patent number: 5025033
    Abstract: A cholinesterase inhibiting agent which contains an alkylene diamine of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is a hydrogen atom or a hydrocarbon residue which may optionally be substituted, or R.sup.1 and R.sup.2 combinedly form, together with the adjacent nitrogen atom, a condensed heterocyclic group, R.sup.3 is a hydrogen atom or a hydrocarbon residue or an acyl group which may optionally be substituted and R.sup.4 is a hydrogen atom, or R.sup.3 and R.sup.4 combinedly form a group of the formula ##STR2## or --(CH.sub.2).sub.m+1 -- (m being 0, 1 or 2), A is --(CH.sub.2).sub.l -- (l being 0, 1 or 2) or --CH.dbd.CH--, X is a substituent or substituents and n is an integer of 4 to 7, or a salt thereof, which are useful as cerebral function improving agents for the prevention or treatment of senile dementia, Alzheimer's disease, Huntington's chorea, hyperkinesia, mania and so forth.
    Type: Grant
    Filed: January 25, 1989
    Date of Patent: June 18, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Akinobu Nagaoka
  • Patent number: 5025005
    Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: June 18, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
  • Patent number: 5001115
    Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: March 19, 1991
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4985452
    Abstract: A fungicifdal composition comprising a fungicidally effective amount of (i) a substituted 1-hydroxyethyl-triazole of the formula ##STR1## in which A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--,or an addition product thereof with an acid or metal salt, and (ii) at least one member selected from the group consisting of(A) wettable sulphur,(B) a polyhalogenoalkylthio derivative,(C) a quanidine derivative,(D) an aromatic carboxylic acid derivative(E) a dithiocarbamate,(F) a benzimidazole derivative,(G) an imidazole or triazole derivative,(H) a phosphoric acid ester,(I) a tetrahydroquinoline derivative,(J) an S,N-heterocyclene compound,(K) a urea derivative,(L) a sulphonamide derivative,(M) a polyhydroxy ether derivative,(N) a triazine derivative,(O) a copper complex salt,(P) an N-formyl derivative,(Q) a morpholine derivative,(R) a quinoxaline derivative, and(S) a dicarboximide derivative.
    Type: Grant
    Filed: November 20, 1989
    Date of Patent: January 15, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans Scheinpflug, Graham Holmwood
  • Patent number: 4975425
    Abstract: Foam compositions containing a herbicide or pesticide which are readily absorbed systemically by plant life are made by incorporating a gas such as air into a composition made up of an alcohol, a modified coconut acid or a blend of nonionic and anionic surfactants, water and a systemic herbicide or pesticide. These foam compositions are applied directly to plant life such as trees and are absorbed within three minutes, often within one minute.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: December 4, 1990
    Assignee: Mobay Corporation
    Inventor: Horace G. Barnett, Jr.
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4950682
    Abstract: The present invention relates to synergistic arthropodicidal composition of several pyrethroidal active ingredients causing no damage to warm-blooded organisms comprising pyrethroides and piperonyl butoxide as active ingredient which comprises as pyrethroidal active ingredient 0.1-20% by weight of 1StransR-alpha-cyano-3-phenoxy-benzyl-3- (2,2-dichlorvinyl)-2,2-dimethyl/cyclopropane-cyrboxylate of the Formula I ##STR1## 0.05-10% by weight of cis-trans-tetramethrin (3,4,5,6-tetrahydrophthalimido-methyl(1RS)-cis-trans-chrysantemate) or trans-tetramethrin of the Formula II ##STR2## and a further pyrethroide, 0.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: August 21, 1990
    Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.
    Inventors: Laszlo Pap, Peter Sarkozi, Eva Somfai, Andras Szego, Istvan Szekely, Gyorgy Hidasi, Sandor Zoltan, Aniko Deak nee Moinar, Agnes Hegedus, Bela Bertok, Sandor Botar, Antal Gajary, Lajos Nagy
  • Patent number: 4933360
    Abstract: Water-soluble dispersions of chlorthalidone are prepared by a process comprising:(a) forming a solution comprising a water soluble pharmaceutically acceptable polymeric carrier and a C.sub.1 -C.sub.4 alkanol,(b) dissolving chlorthalidone in the solution thus formed, and(c) removing the C.sub.1 -C.sub.4 alkanol from the solution by evaporation,the amount of said carrier being effective to suppress substantially the formation of the alkyl ether by-product from the reaction of chlorthalidone with the C.sub.1 -C.sub.4 alkanol. A preferred water soluble carrier is polyvinylpyrrolidone and a preferred C.sub.1 -C.sub.4 alkanol is methanol.
    Type: Grant
    Filed: November 8, 1985
    Date of Patent: June 12, 1990
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Nivedita Pandit, Stephen T. Horhota
  • Patent number: 4923888
    Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 acylamino group;R.sub.1 means hydrogen or a carboxyl-protective group; andR.sub.2 represents a --(CH.sub.2).sub.n --CO.sub.2 R.sub.5 group, whereinn is 1, 2, 3 or 4; andR.sub.5 stands for hydrogen or a carboxyl-protective group; orR.sub.2 means a --(CH.sub.2).sub.n --NH.sub.2 group, whereinn is 1, 2, 3 or 4of E and/or Z configurtion as well as their salts.The compounds according to the invention show a cytoprotective effect and promote the healing of the stomach ulcer. Their toxicity is low.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: May 8, 1990
    Assignee: Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Tamas Fodor, Laaszlo Dobay, Jaanos Fischer, Bela Stefkoo, Elemeer Ezer, Judit Matuz, Katalin Saghy, Laaszlo Szporny
  • Patent number: 4886824
    Abstract: The invention relates to plant protection compositions based on a two-component system of plant fungicides, one of which is 1-[2-(2,4-dichlorophenyl)pentyl]-1H-1,2,4-triazole and the other is an N-haloalkanesulfenylphthalimide derivative.In the range from 1:3 to 1:100 the disclosed mixtures display enhanced fungicidal activities.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: December 12, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Wilhelm Ruess, Pierre Urech, Jurg Eberle, Theodor Staub
  • Patent number: 4883806
    Abstract: Novel isomers and mixtures thereof of cyclopropane carboxylic acid derivatives with a 3-unsaturated side chain of the formula ##STR1## wherein A' is selected from the group consisting of (1) alkyl of 1 to 18 carbon atoms, (2) benzyl optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, alkadienyl of 4 to 8 carbon atoms, methylenedioxy or halogen, ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --C.tbd.CH and monocyclic aryl, ##STR3## wherein a is selected from the group consisting of hydrogen and methyl and R.sub.3 is an aliphatic group of 2 to 6 carbon atoms containing at least one carbon-carbon unsaturation ##STR4## wherein a and and R.sub.3 have the above definition and R.sub.1 ' and R.sub.
    Type: Grant
    Filed: September 23, 1987
    Date of Patent: November 28, 1989
    Assignee: Roussel Uclaf
    Inventors: Jacques Martel, Jean Tessier, Andre Teche
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4853407
    Abstract: Compounds represented by formula ##STR1## wherein Y.sup.1 and Y.sup.2 are identical or different, and respectively denote benzoylamino groups or phthalimide groups. This compound is useful for inhibition of dipeptidase.
    Type: Grant
    Filed: May 20, 1988
    Date of Patent: August 1, 1989
    Assignee: Sanraku Incorporated
    Inventors: Norio Shibamoto, Takeo Yoshioka, Yasuo Fukagawa, Tomoyuki Ishikura
  • Patent number: 4851421
    Abstract: The invention relates to a biocidal fine powder with increased biocidal activity and an agricultural suspension containing the biocidal fine powder and an adjuvant selected from the group consisting of polyoxyalkylene-type nonionic surface active agents and polyoxyalkylene alkyl or alkylaryl ether phosphates or their salts.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: July 25, 1989
    Assignee: Kao Corporation
    Inventors: Tetsuji Iwasaki, Yasushi Kamihisa
  • Patent number: 4847301
    Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.
    Type: Grant
    Filed: July 27, 1988
    Date of Patent: July 11, 1989
    Assignee: Pennwalt Corporation
    Inventor: Robert J. Murray
  • Patent number: 4839378
    Abstract: Fluorophthalimide compounds represented by the following general formula (I): ##STR1## wherein R each stands for an ethyl group or an isopropyl group, are effective for controlling diseases of agricultural plants, especially diseases caused by microorganisms belonging to the genus Rhizoctonia, represented by sheath blight of rice plants, and diseases caused by Basidomycetes.
    Type: Grant
    Filed: April 28, 1987
    Date of Patent: June 13, 1989
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Masao Koyama, Michiaki Iwata, Kunihiko Kurihara, Masaji Sezaki
  • Patent number: 4801603
    Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: January 31, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
  • Patent number: 4795757
    Abstract: Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.
    Type: Grant
    Filed: November 20, 1986
    Date of Patent: January 3, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
  • Patent number: 4737512
    Abstract: Novel 4-(substituted-isoindol-2-yl)phenoxy-pentanoic and -heptanoic acids and derivatives which are useful as anti-arteriosclerotic agents are disclosed. The compounds elevate the high density lipoprotein fraction of cholesterol and also lower the low density lipoprotein fraction of cholesterol. Methods for preparing and using the compounds are included.
    Type: Grant
    Filed: October 27, 1986
    Date of Patent: April 12, 1988
    Assignee: Warner-Lambert Company
    Inventor: Milton L. Hoefle